posted on 2024-01-10, 19:42authored byZhenguo Zhang, Lanyang Li, Hailun Xu, Chi-Lik Ken Lee, Zhenhua Jia, Teck-Peng Loh
A new
bioconjugation reagent containing silicon has been developed
for the selective reaction with thiols. The inclusion of silicon significantly
improves chemoselectivity and suppresses retro processes, thereby
exceeding the capabilities of traditional reagents. The method is
versatile and compatible with a broad range of thiols and unsaturated
carbonyl compounds and yields moderate to high results. These reactions
can be conducted under biocompatible conditions, thereby making them
suitable for protein bioconjugation. The resulting conjugates display
good stability in the presence of various biomolecules, which suggests
their potential application for the synthesis of antibody–drug
conjugates. Furthermore, the presence of a silicon moiety within the
conjugated products opens up new avenues for drug release and bridging
inorganics with other disciplines. This new class of silicon-containing
thiol-specific bioconjugation reagents has significant implications
for researchers working in bioanalytical science and medicinal chemistry
and leads to innovative opportunities for advancing the field of bioconjugation
research and medicinal chemistry.